Furosemide - instructions for use, dose, side effects, contraindications

High-speed diuretic with pronounced diuretic effect. Disrupts the reabsorption of sodium, chlorine ions in the thick segment of the ascending loop of Henle. Furosemide has a pronounced diuretic, natriuretic, chlororetic effect. In addition, it increases the excretion of potassium, calcium, and magnesium ions. With heart failure quickly leads to a decrease in preload on the heart through the expansion of large veins. It has an antihypertensive effect, due to an increase in the elimination of sodium chloride and a decrease in the response of the smooth muscles of the vessels to vasoconstrictive effects and as a result of a decrease in the volume of circulating blood.With intravenous administration, the action of furosemide develops in 15-20 minutes and reaches a maximum at the end of the first hour; the diuretic effect continues for 3 hours, with reduced renal function - up to 8 hours.

During the period of action, excretion of sodium ions increases significantly, however, after its termination, the elimination rate decreases below the initial level ("rebound" or "cancel" syndrome). The phenomenon is caused by a sharp activation of the renin-angiotensin and other antinatriuretic neurohumoral regulating units in response to massive diuresis.

Pharmacokinetics:

Time of achievement. the maximum concentration for intravenous administration is 30 minutes. The relative volume of the distribution is 0.2-l / kg. Furosemide on 98% is associated with blood plasma proteins, mainly with albumins. Penetrates through the placental barrier, excreted in breast milk.

Metabolised in the liver with formation, with the formation of 4-chloro-5-sulfamoyl-anthranilic acid. It is secreted into the lumen of the renal tubules through the anion transport system that is located in the proximal compartment. The half-life of furosemide after intravenous administration is 0.5 to 1 hour. Bioavailability of 60-70%.To be excreted mainly (88%) by the kidneys in the unaltered form and in the form of metabolites; through the intestine - 12%. Clearance - 1,5-3 ml / min / kg.

With renal failure, the excretion of furosemide slows down, and the half-life increases; with severe renal failure, the final half-life can increase up to 24 hours.

With hemodialysis and peritoneal dialysis furosemide output is insignificant.

In liver failure, the half-life of furosemide is increased by 30-90%, mainly due to an increase in the volume of distribution. Pharmacokinetic parameters in this category of patients can vary greatly.

With chronic heart failure, severe degree of arterial hypertension and in elderly patients excretion, furosemide slows down due to decreased kidney function.

In preterm premature infants, furosemide excretion may be slowed down, which depends on the degree of maturity of the kidneys, the metabolism of the drug in infants can also be slowed down, since their glucuronizing ability is inferior. In children, whose age after conception exceeds 33 weeks, the final half-life does not exceed 12 hours.In infants at the age of two months and older, excretion of furosemide does not differ from that in adults.

Indications:

Otecny, syndrome with chronic heart failure, edematous syndrome with acute heart failure, edematous syndrome with chronic renal failure, acute renal failure, edematous syndrome with nephrotic syndrome (with nephrotic syndrome, in the foreground is the treatment of the underlying disease); edematous syndrome with liver disease, cerebral edema, hypertensive crisis, maintenance of forced diuresis in case of poisoning with chemical compounds, excreted kidneys in unchanged form.

Contraindications:

Hypersensitivity to furosemide and other components of the drug, in patients with allergies to sulfonamides (sulfanilamide antimicrobial agents or sulfonylureas), a cross allergy may develop furosemide, acute glomerulonephritis, acute renal failure with anuria (glomerular filtration value less than 3-5 ml / min), severe hepatic insufficiency, hepatic coma and precoma, pronounced violations of urinary outflow of any etiology,(including, unilateral urinary tract damage) hyperuricemia, gout; decompensated mitral or aortic stenosis, increased central venous pressure, (over 10 mm Hg), idiopathic hypertrophic subaortic stenosis, violation of water-electrolyte metabolism and acid-base balance (hypokalemia, alkalosis, hypovolemia, hyponatremia, hypochloremia, hypocalcemia, hypomagnesemia), digitalis intoxication.

Carefully:

Arterial hypotension in conditions in which excessive reduction in blood pressure is particularly dangerous (stenosing lesions of the coronary and / or cerebral arteries); with acute myocardial infarction (increased risk of cardiogenic shock); with latent or manifested diabetes mellitus (decreased glucose tolerance); gout; with hepatorenal syndrome; with hypoproteinemia (risk; development of ototoxicity); with a violation of the outflow of urine (benign prostatic hyperplasia, narrowing of the urethra or hydronephrosis); with hearing loss; pancreatitis,diarrhea; with ventricular arrhythmias in the anamnesis; with systemic lupus erythematosus; in premature babies; children (the possibility of forming calcium-containing kidney stones (nephrolithiasis) and the deposition of calcium salts in the kidney parenchyma, (nephrocalcinosis), so regular monitoring of kidney function and ultrasound examination of the kidneys is necessary).

Pregnancy and lactation:

Furosemide penetrates through the placental barrier, so the drug should not be administered during pregnancy. If for vital reasons furosemide is prescribed to pregnant women, careful monitoring of the fetus is necessary.

If you need to use the drug during lactation at the time of treatment should stop breastfeeding.

Dosing and Administration:

Furosemide prescribe intravenously, (slowly - struyno) if impossible - intramuscularly (when intravenous injection or application of the drug inside) is impossible.

It is recommended to use the smallest doses of the drug, sufficient to achieve the necessary therapeutic effect.

Intravenous administration of furosemide is carried out, when taking the drug inside is impossible or there is a violation of absorption of the drug in the small intestine or in urgent situations.

The question of the duration of treatment is decided by the doctor, given the nature and severity of the disease. After the onset of the desired effect, go on to take the drug inside. When administered intravenously, the drug should be administered slowly. The rate of intravenous administration should not exceed 4 mg per minute.

In patients with severe renal failure (serum creatinine> 5 mg / dl), it is recommended that the rate of administration does not exceed 2.5 mg per minute. The drug is administered in doses of 20-40 mg. 1-2 times a day; in the absence of a diuretic response every 2 hours, injected in an enlarged 50% dose until an adequate diuresis is achieved. Patients with reduced glomerular filtration and low diuretic response are prescribed in large doses of 1-1.5 g. In children, the initial single dose of the drug is 1 mg / kg (0.1 ml / kg) of body weight slowly for 1 to 2 minutes (0.5 ml / kg per minute). The maximum daily dose for intravenous administration in children is 6 mg / kg.

Side effects:

From the cardiovascular system: lowering blood pressure (BP), collapse, tachycardia, arrhythmia, a decrease in the volume of circulating blood, thrombophlebitis, orthostatic hypotension.

FROMo side of the nervous system: dizziness, headache, muscle, weakness, convulsions.calf muscles (tetany), paresthesia, - apathy, adynamia, weakness, lethargy, drowsiness, confusion.

From the senses: visual and hearing impairments, tinnitus.

From the gastrointestinal tract, liver: anorexia, dry mouth, thirst, nausea, vomiting, diarrhea, constipation; Cholestatic jaundice, pancreatitis (exacerbation).

On the part of the genitourinary system: oliguria, acute retention of urine (in patients with benign prostatic hyperplasia, narrowing of the urethra), interstitial nephritis, hematuria, impotence, renal calcification in premature infants.

Allergic reactions: purpura, urticaria, exfoliative dermatitis, erythema multiforme, vasculitis, necrotizing angiitis, itching, chills, fever, photosensitivity, anaphylactic shock and toxic epidermal necrolysis; Stevens-Johnson syndrome.

On the part of the hemopoiesis: leukopenia, thrombocytopenia, agranulocytosis, eosinfbelia, aplastic anemia, hemolytic anemia.

On the part of water-electrolyte metabolism: hypovolemia, dehydration (risk of thrombosis and thromboembolism), hypokalemia, hyponatremia, (hypochloraemia, hypocalcemia, hypomagnesemia, metabolic alkalosis.

Laboratory indicators: hyperglycemia, hypercholesterolemia, hypertriglyceridemia, increased creatinine and urea concentration in the blood, decreased glucose tolerance, manifestation of latent diabetes mellitus, hyperuricemia, glucosuria, hypercalciuria.

Preterm infants during the first weeks of life furosemide may increase the risk of Botallov duct preservation, increase in activity of "liver" transaminases.

Possible local pain reaction in the place of intramuscular injection.

Overdose:

Symptoms: a decrease in blood pressure, collapse, shock, hypovolemia, dehydration, hemoconcentration, arrhythmias, acute renal failure with anuria, thrombosis, thromboembolism, drowsiness, confusion, flaccid paralysis, apathy.

Treatment: correction of water-salt balance and acid-base state, correction of hematocrit, replenishment of circulating blood volume, symptomatic treatment. There is no specific antidote.

Interaction:

Increases the concentration and risk of nephro- and ototoxic effects of cephalosporins, aminoglycosides, chloramphenicol, ethacrynic acid, cisplatinum, amphotericin B (due to competitive renal excretion).

Increases the effectiveness of diazoxide and theophylline, reduces - hypoglycemic agents, allopurinol.

Pressor amines and furosemide mutually reduce efficiency.

Drugs that block tubular secretion, increase the concentration of furosemide in serum.

With the simultaneous use of glucocorticosteroids, amphotericin B increases the risk of hypokalemia, with cardiac glycosides - the risk of developing digitalis intoxication due to hypokalemia (for high and low-polar) and elongation of the half-life (for low-polarity) increases.

Reduces renal clearance of lithium preparations and increases the likelihood of development of intoxication. Non-steroidal anti-inflammatory drugs, sucralfate reduce the diuretic effect due to inhibition of prostaglandin synthesis, renin level in the blood plasma and elimination of aldosterosis.

Strengthens the antihypertensive effect of antihypertensive drugs, neuromuscular blockade of depolarizing muscle relaxants (succinylcholine) and weakens the effect of nondepolarizing muscle relaxants (tubocurarine).

Simultaneous reception of large doses of salicylates against furosemide therapy increases the risk, manifestations of their toxicity (due to competitive renal excretion).

The appointment of angiotensin converting enzyme (ACE) inhibitors or antagonists; receptors of angiotensin II to patients previously treated with furosemide, may lead to impaired renal function, and in some cases to the development of acute renal failure. It is recommended to cancel furosemide, or reduce the dose of furosemide 3 days before the start of therapy; ACE inhibitors or angiotensin II receptor antagonists.

The simultaneous use of probenicide or methotrexate may decrease the effectiveness of furosemide (the same pathway of secretion). On the other hand furosemide can lead to a decrease in renal elimination of these drugs.

Intravenously administered furosemide has a slightly alkaline reaction, so it can not be mixed with drugs with a pH of less than 5,5.

Special instructions:

Before the beginning of therapy with the drug should be excluded from the presence of severe violations of urine outflow, patients with partial disturbance of urine outflow need careful observation; thepremature babies require regular monitoring of the function, kidney and ultrasound of the kidneys.

Against the background of course treatment, it is necessary to periodically monitor blood pressure, blood plasma electrolytes, acid-base state of residual nitrogen, uric acid creatinine, liver function and, if necessary, appropriate correction of treatment (with higher multiplicity in patients with frequent vomiting and parenterally injected fluids) .

Patients with hypersensitivity to sulfonamides and sulfonylureas may have cross-sensitivity to furosemide.

Patients receiving high doses of furosemide, in order to avoid the development of hyponatremia and metabolic alkalosis, it is not advisable to limit the intake of table salt.

For the prevention of hypokalemia, the simultaneous administration of potassium and potassium-sparing diuretics (primarily spironolactone) is recommended, as well as adherence to a diet rich in potassium.

An increased risk of violations, water-electrolyte balance is noted in patients with renal insufficiency.

Selection of dosing regimen in patients with ascites on the background of liver cirrhosis should be performed in a hospital (violation vodnoelektrolitnogo balance may lead to the development of hepatic coma).

This category of patients shows regular monitoring of the content of plasma electrolytes.

When azotemia and oliguria appear or increase in patients with severe progressive kidney disease, it is recommended to suspend treatment.

It is allocated with milk in women during lactation, in connection with which it is advisable to stop feeding.

In patients with diabetes, diabetes or with reduced glucose tolerance, periodic monitoring of glucose levels in the blood and urine is required.

In patients in an unconscious state, with benign prostatic hyperplasia, or narrowing of the ureters, hydronephrosis, requires monitoring of urine output due to the possibility of acute urinary retention.

Effect on the ability to drive transp. cf. and fur:

During the treatment period, it is necessary to refrain from driving vehicles and practicing other potentially hazardous activities that require an increased concentration of attention and speed of psychomotor reactions.

Form release / dosage:

Solution for intravenous and intramuscular injection 10 mg / ml

2 ml per ampoule of neutral glass.

Packaging:

For 10 ampoules with instruction for use and a knife for opening ampoules or a scarifier ampullum is placed in a box of cardboard.

5 or 10 ampoules are placed in a contour mesh package made of a polyvinylchloride film or polyethylene terephthalate tape and aluminum foil or paper with a polyethylene coating or without a foil, or without paper.

For 1 or 2 contour packs with instructions for use and a knife for opening ampoules or a scarifier ampullum is placed in a pack of cardboard.

When you pack the ampoules with a break ring or break point, the ampoule opener or ampoule scapper is not put in.

Storage conditions:

In the dark place at a temperature of 15 to 25 ° C.

Keep out of the reach of children.

Shelf life:

2 years. Do not use after the expiration date.

Terms of leave from pharmacies:On prescription

Registration number:P N000360 / 01

Date of registration:26.09.2011

The owner of the registration certificate:NOVOSIBHIMFARM, OJSC NOVOSIBHIMFARM, OJSC Russia

Manufacturer: & nbsp

NOVOSIBHIMFARM, OJSC Russia

Representation: & nbspNOVOSIBHIMFARM, OJSCNOVOSIBHIMFARM, OJSC

Information update date: & nbsp13.11.2015

Illustrated instructions

Instructions

Furosemide (Furosemide )